NH125

NH125 is a potent and selective inhibitor of eukaryotic elongation factor 2 kinase (eEF-2K/CaMKIII), also can induce eEF2 phosphorylation, with an IC₅₀ of 60 nM for eEF-2K^[1][2]. IC50 & Target: IC50: 60 nM (eEF-2K/CaMKIII)^[1]. In Vitro: NH125 inhibits eEF-2 kinase activity (IC₅₀ = 60 nM) in vitro, blocks the phosphorylation of eEF-2 in intact cells, and shows relative selectivity over other protein kinases: protein kinase C (IC₅₀ = 7.5 μM), protein kinase A (IC₅₀ = 80 μM), and calmodulin-dependent kinase II (IC₅₀ > 100 μM). NH125 decreases the viability of 10 cancer cell lines with IC₅₀s ranging from 0.7 to 4.7 μM. Forced overexpression of eEF-2 kinase in a glioma cell line produces 10-fold resistance to NH125. In conclusion, these results suggest that identification of potent inhibitors of eEF-2 kinase may lead to the development of new types of anticancer drugs^[1]. Anticancer effect of NH125 is not mediated through inhibition of eEF2K. Inhibition of cell growth correlates with induction of peEF2^[2].